^ abcdefgF.C. Tuwunay; M. Orme (6 December 2012). European Cowwaboration: Towards Drug Devewopement [sic] and Rationaw Drug Therapy: Proceedings of de Sixf Congress of de European Association for Cwinicaw Pharmacowogy and Therapeutics Istanbuw, June 24–28, 2003. Springer Science & Business Media. pp. 107–. ISBN978-3-642-55454-4. Investigation of de Pharmacokinetics and Metabowism of Promegestone in Heawdy Femawe Vowunteers Fowwowing Singwe Oraw Administration of 1 mg Promegestone I Guawano V., 1Geneteau A., I Chassard D., I Fordham P., 2Schatz B. I Aster-Cephac, 3/5, Rue Eugene Miwwon, 75015 Paris, France 2Laboratoire Aventis, 46 Quai De La Rapee, F-75601 Paris Cedex 12, France. A singwe 1 mg oraw dose of promegestone (Surgestonee, 2x0.5 mg) was given to 12 heawdy premenopausaw women, uh-hah-hah-hah. The aims were to determine de concentrations of promegestone and its metabowites and deir pharmacokinet-ic parameters. Bwood and urine sampwes were fowwowed untiw 96 hours post dose. To avoid any interference wif naturaw hormones, promegestone was given between day 7 and 10 of de menstruaw cycwe. Cwinicaw safety and towerabiwity were good. Most of de minor adverse events observed were estimated possibwy winked to de study drug (menstruaw disorders) because cwassicawwy rewated to progestins derapy. In addition, no cwinicawwy rewevant biowogicaw modifications were observed. There was a stereosewective metabowism of promegestone in favor of de 21S hydroxy-promegestone, de main circuwating compound in pwasma (AUC ratio 5/R of about 21). Levews of 21S hydroxy-promegestone are about twice greater dan dat of unchanged promegestone. The pwasma wevews of de second metabowite, i.e. 21 R hydroxy-promegestone are far bewow dese of eider promegestone and 21S hydroxy-promegestone. Promegestone, 215 hydroxy- and 21R hydroxy-promegestone are not excreted in urine. About 3% of de dose was recov-ered in urine as suwfo and/or gwucuro-conjugate 21S hydroxy-promegestone and about 1% of de dose as suwfo and/or gwucuro conjugate 21R hydroxy-promegestone.